Study On Design Synthesis And Bioactivity Of Ferrocenesulfonylureas (Ferrocenesulfonamides)

Acetolactate synthase enzyme (ALS) inhibitors are one of the mostimportant classes of herbicides used for selective weed control in variety ofcrops. They can inhibit weeds growth or kill weeds which interfere withbranched-chain amino acids by inhibiting ALS activity in plants. The attributeof low application rate, good crop selectivity, environmental safety andcompatibility with the trend towards post-emergence weed control exhibitedby these compounds are important characteristics for modern agrochemicals,which have led to the rapid success of ALS inhibitors as herbicidal productsand attracted a world-wide research commitment. Over the past two decades,thirteen structurally diverse classes of ALS inhibitors including herbicides ofsulfonylurea, imidazolinone, sulfonamide and pyrimidylsalicylate have beenfound, and much effort is being put into finding new classes.In this thesis, the creative processes of sulfonylurea and sulfonamideherbicides were described. The research progress of ALS, structure-activityand theoretical research of sulfonylurea and sulfonamide herbicides were alsoreviewed. Two series of novel ferrocenesulfonylurea (ferrocenesulfonamide)including twelve compounds were synthesized from ferrocenesulfonylamideand 2-amino -substitued pyrimidine. Their structures were confirmed byelemental analysis, 1^HNMR and IR. Many reactions were discussed andimproved the yield of.the title compound Spectrums of compounds wereanalyzed.The herbicidal activity was determined to rape and results showed thatsome compounds have good activity. Among of them, the activity of N-( 4,6–dimethylpyrimidin-2-yl ) ferrocenesulfonylureas is the best. The inhibitingactivity to rape of compoundsâ… ₅ andâ… ₆ of different concentrations weremeasured and their regression formulas,LC50 were calculated. The bioassary ofcompoundsâ…¡_1-3 for antifungal activity was carried out and the all the titlecompounds were found to be high activity against rice sheath blight .The crystal structures of compounds â…¡₂ were determined by X-ray...